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Some tips on 438631-77-7

438631-77-7, 438631-77-7 (R)-1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate 6558432, apiperazines compound, is more and more widely used in various fields.

438631-77-7, (R)-1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To degassed solution of 68 1,4-dioxane (71.6 mL) and 56 DIPEA (5.65 mL, 32.46 mmol) at rt was added 505 7-bromo-4-chloro-6,8-difluoro-3-nitroquinoline (3.5 g, 10.82 mmol) followed by 272 1-tert-butyl 3-methyl (3R)-piperazine-1,3-dicarboxylate (3.96 g, 16.23 mmol). The reaction was heated at 100 C. for 16 h. The reaction was cooled to rt and the solvent removed in vacuo. The resulting residue was diluted with EtOAc (300 mL), washed with water (2¡Á250 mL) and brine (100 mL). The organic layer was dried (phase separator) and concentrated in vacuo to afford crude material which was purified by flash silica chromatography (0 to 50% 57 EtOAc in 58 heptane) to give 507 1-tert-butyl 3-methyl (3R)-4-(7-bromo-6,8-difluoro-3-nitroquinolin-4-yl)piperazine-1,3-dicarboxylate (3.89 g, 68%) as an orange dry film; 1H NMR (400 MHz, DMSO, 30 C.) 1.45 (9H, s), 3.18-3.29 (2H, m), 3.54 (3H, s), 3.57-3.66 (1H, m), 3.72-3.95 (2H, m), 4.05 (1H, s), 4.33 (1H, s), 8.06 (1H, dd), 9.13 (1H, s); m/z: ES+ [M+H]+ 530.9.

438631-77-7, 438631-77-7 (R)-1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate 6558432, apiperazines compound, is more and more widely used in various fields.

Reference£º
Patent; ASTRAZENECA AB; Kettle, Jason Grant; Bagal, Sharanjeet; Robb, Graeme Richard; Smith, James Michael; Goldberg, Frederick Woolf; Cassar, Doyle Joseph; Feron, James Lyman; US2019/177338; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

New learning discoveries about (R)-1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate

As the paragraph descriping shows that 438631-77-7 is playing an increasingly important role.

438631-77-7, (R)-1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,438631-77-7

DIPEA (5.15 mL, 29.46 mmol) was added to 695 7-bromo-4,5,6-trichloro-3-nitroquinoline (3.5 g, 9.82 mmol) and 272 1-(tert-butyl) 3-methyl (R)-piperazine-1,3-dicarboxylate (4.8 g, 19.64 mmol) in 78 THF (50 mL) at rt. The resulting solution was stirred at 80 C. for 2 days. The solvent was removed in vacuo. The crude product obtained was purified by flash silica chromatography (0 to 20% 57 EtOAc in 148 petroleum ether) to afford 697 1-tert-butyl 3-methyl (3R)-4-(7-bromo-5,6-dichloro-3-nitroquinolin-4-yl)piperazine-1,3-dicarboxylate (1.95 g, 35%) as a red solid; 1H NMR (400 MHz, DMSO, 30 C.) 1.44 (9H, s), 3.25-3.32 (3H, m), 3.50-3.60 (2H, m), 3.75-3.85 (2H, m), 3.98-4.04 (1H, m), 4.12-4.22 (2H, m), 7.80-7.95 (1H, m), 9.07 (1H, d); m/z: ES+ [M+H]+=563.

As the paragraph descriping shows that 438631-77-7 is playing an increasingly important role.

Brief introduction of 438631-77-7

The synthetic route of 438631-77-7 has been constantly updated, and we look forward to future research findings.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.438631-77-7,(R)-1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate,as a common compound, the synthetic route is as follows.

Bromobenzene (125 mg, 0.8 mmol), 1-tert-butyl 3-methyl (3R)-piperazine-1,3-dicarboxylate (213.94 mg, 0.88 mmol), Pd2(dba)3.CHCl3 (8.24 mg, 0.01 mmol), RuPhos (9.29 mg, 0.02 mmol) and Cs2CO3 (324.24 mg, 1 mmol) were suspended in anhydrous toluene (2.5 ml). The sealed reaction was heated at 110 C. for 18 h. The reaction was partitioned between DCM (5 ml) and water (5 ml) then the organics were separated and concentrated in vacuo. The residue was purified via flash column chromatography using a gradient of 0% to 100% EtOAc in heptane then 0% to 100% MeOH in EtOAc. Fractions containing product were combined and concentrated in vacuo to yield the title compound as a yellow glassy solid (51 mg, 13%). LCMS Method 2-Tr=1.21 min (ES+) (M+H+) 321.0., 438631-77-7

The synthetic route of 438631-77-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Navitor Pharmaceuticals, Inc.; O’Neill, David John; Saiah, Eddine; Kang, Seong Woo Anthony; Brearley, Andrew; Bentley, Jonathan; (519 pag.)US2018/127370; (2018); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Some tips on 438631-77-7

438631-77-7, 438631-77-7 (R)-1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate 6558432, apiperazines compound, is more and more widely used in various fields.

438631-77-7, (R)-1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

DIPEA (1.79 ml, 10.25 mmol) was added to a solution of 3-bromo-8-chloro-2,4-dimethyl-7-nitro-1,5-naphthyridine (2.95 g, 9.32 mmol) and 1-tert-butyl 3-methyl (3R)-piperazine-1,3-dicarboxylate (2.39 g, 9.79 mmol) in THF (40 ml). The resultant brown solution was heated at 65 C. for 24 h. The reaction mixture was concentrated in vacuo, the residue re-dissolved in ethyl acetate and washed with water (*2) and brine. The aqueous layer was back extracted with ethyl acetate and the combined organics dried (phase separator) and concentrated in vacuo to afford crude material as a brown foam. This was purified by flash silica chromatography (0 to 100% ethyl acetate in heptane) to afford 1-tert-butyl 3-methyl (3R)-4-(7-bromo-6,8-dimethyl-3-nitro-1,5-naphthyridin-4-yl)piperazine-1,3-dicarboxylate (4.13 g, 85%) as a yellow solid; 1H NMR (400 MHz, DMSO, 30 C.) 1.42 (9H, s), 2.74 (3H, s), 2.82 (3H, s), 3.09-3.15 (1H, m), 3.24 (1H, s), 3.55 (1H, d), 3.67 (3H, s), 3.73-3.84 (1H, m), 3.88 (1H, s), 4.37 (1H, d), 5.59 (1H, s), 9.04 (1H, s); m/z: ES+ [M+H]+ 523.9.

438631-77-7, 438631-77-7 (R)-1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate 6558432, apiperazines compound, is more and more widely used in various fields.

Analyzing the synthesis route of 438631-77-7

The synthetic route of 438631-77-7 has been constantly updated, and we look forward to future research findings.

438631-77-7, (R)-1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 3; 4-(5-Trifluoromethyl-pyridin-2-yl)-piperazine-l,3-dicarboxylic acid 1-tert-butyl ester 3-methyl ester :; S-Methyl-piperazine-l^-dicarboxylic acid 1-tert-butyl ester (120 mg, 0.49 mmol) and 2-Bromo-5- trifluoromethyl-pyridine (133 mg, 0.59 mmol) were dissolved in 2.0 mL of anhydrous toluene (degassed). In a separate, septum-equipped vial were placed tri(dibenzylideneacetone)dipalladium (0) (22 mg, 0.024 mmol), l,3-bis(2,6-di-J-propylphenyl)imidazolium chloride (42 mg, 0,1 mmol) and sodium ^-butoxide (57 mg, 0.59 mmol). This “catalytic” vial was equipped with a magnetic stir bar and flushed with dry nitrogen. The reactant solution was next transferred to the “catalytic” vial and the mixture was stirred at 1000C for 5 h. After this period the mixture was combined with 20 mL of hexane/EtOAc (2:1) and was passed through a pad of Celite. The resulting filtrate was evaporated in vacuo and purified using flash silica chromatography (0-20% EtOAc/Hexane) to yield 110 mg (58%) of 4-(5-TrifIuoromethyl-pyridin-2-yl)- piperazine-l,3-dicarboxylic acid 1-tert-butyl ester 3-methyl ester., 438631-77-7

The synthetic route of 438631-77-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; KALYSPSYS, INC.; NOBLE, Stewart A.; OSHIRO, Guy; MALECHA, James W.; ZHAO, Cunxiang; ROBINSON, Carmen K. M.; DURON, Sergio G.; SERTIC, Michael; LINDSTROM, Andrew; SHIAU, Andrew; BAYNE, Christopher; KAHRAMAN, Mehmet; LOU, Boliang; GOVEK, Steven; WO2006/55187; (2006); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Simple exploration of 438631-77-7

438631-77-7 (R)-1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate 6558432, apiperazines compound, is more and more widely used in various.

1-tert-Butyl 3-methyl (3R)-piperazine-1,3-dicarboxylate (5.03 g, 20.59 mmol) was added to 670 7-bromo-4,6-dichloro-5-fluoro-3-nitroquinoline (3.5 g, 10.30 mmol) and 56 DIPEA (7.19 mL, 41.19 mmol) in 78 THF (50 mL) at rt. The resulting solution was stirred at 80 C. for 16 h. The solvent was removed in vacuo. The crude product obtained was purified by flash silica chromatography (0 to 20% 57 EtOAc in 148 petroleum ether) to afford 672 1-tert-butyl 3-methyl (3R)-4-(7-bromo-6-chloro-5-fluoro-3-nitroquinolin-4-yl)piperazine-1,3-dicarboxylate (1.75 g, 31%) as a red solid; 1H NMR (300 MHz, DMSO, 30 C.) 1.45 (9H, s), 3.31 (3H, d), 3.37-3.45 (2H, m), 3.47-3.55 (2H, m), 3.68-3.82 (2H, m), 4.20-4.30 (1H, m), 8.45 (1H, d), 9.10 (1H, s); m/z: ES+ [M+H]+=547

438631-77-7 (R)-1-tert-Butyl 3-methyl piperazine-1,3-dicarboxylate 6558432, apiperazines compound, is more and more widely used in various.